RESUMO
Transdermal transport is now becoming one of the most convenient and safe pathways for drug delivery. In some cases it is necessary to use skin penetration enhancers in order to allow for the transdermal transport of drugs that are otherwise insufficiently skin-permeable. A series of oleanolic acid amides as potential transdermal penetration enhancers was formed by multistep synthesis and the synthesis of all newly prepared compounds is presented. The synthetized amides of oleanolic acid were tested for their in vitro penetration promoter activity. The above activity was evaluated by means of using the Fürst method. The relationships between the chemical structure of the studied compounds and penetration activity are presented.
Assuntos
Amidas/farmacologia , Ácido Oleanólico/farmacologia , Absorção Cutânea/efeitos dos fármacos , Amidas/síntese química , Amidas/química , Membranas Artificiais , Pomadas/farmacologia , Ácido Oleanólico/química , Permeabilidade/efeitos dos fármacos , Progesterona/farmacologiaRESUMO
Some new oleanolic acid derivatives with lactame and thiolactame structures in the A- or C-ring were prepared and tested as percutaneous transport promoters in vitro. Their activity was comparable with activity of N-dodecylcaprolactame (Azone). A-Thiolactame derivative of methyl oleanolate (13) was the most effective compound.
Assuntos
Adjuvantes Farmacêuticos/química , Compostos Aza/química , Lactamas/química , Membranas Artificiais , Absorção Cutânea , Triterpenos/química , Adjuvantes Farmacêuticos/síntese química , Administração Cutânea , Compostos Aza/síntese química , Transporte Biológico Ativo , Humanos , Técnicas In Vitro , Lactamas/síntese química , Permeabilidade , Progesterona/química , Relação Estrutura-Atividade , Triterpenos/síntese químicaRESUMO
The subject of the studies was eye drops made of aloe, containing the group of aloe chemical substances of anti-inflammatory use and neomycin sulphate. The aim of the studies was to evaluate the permeability of biologically active aloe substances, determined as aloenin, through synthetic lipophilic and hydrophilic membranes in a standard perfusion apparatus and in vitro verification of the transport possibilities of these substances through the isolated cornea of pig's eye. The permeability process of biologically active aloe substances determined as aloenin, through synthetic lipophilic and hydrophilic membranes, was analyzed using the first-order kinetics. Estimated quotas of permeability rate constant show that the investigated chemical compounds of aloe, included in the eye drops, diffused through the applied membranes. The studies of permeability through isolated pig's cornea proved that biologically active aloe substances could not overcome this biological barrier. On the basis of biopharmaceutical studies it can be concluded that the eye drops containing aloe and neomycin sulphate, due to the lack of permeating abilities through the eye cornea, should be particularly useful in the treatment of inflammations and infections of external parts of the eye, such as conjuctiva, eyelid edges, lacrimal sac and cornea.